Comparative studies on the efficacy of lincomycin and bacitracin for the control of necrotic enteritis in broiler chickens

Background: The present study was conducted to evaluate the efficacy of lincomycin and/or bacitracin for control of experimentally-induced Clostridium perfringens (CP) infection in broiler chickens.Methods: A total of 100 one-day-old Cobb-mixed chicks were divided into five groups (A, B, C, D and E, each of 20 bird). At the 15th day of age, all birds (except group A) were inoculated orally with CP broth culture (109 CFU/mL). Two days later, drugs were orally administered once daily for five consecutive days as follow; Group A and B were left untreated. Group C, D, and E were treated with lincomycin (0.5 g/l), bacitracin (100 mg/l), lincomycin and bacitracin, respectively. The efficacy of used drugs was estimated based on clinical symptoms, body weight, weight gain, feed conversion rate. Hematobiochemical changes were also determined.Results: Necrotic enteritis in broiler chickens induced a significant decrease in body weight, weight gain, erythrocytic count, hemoglobin content, PCV %, serum proteins, catalase, and superoxide dismutase. Additionally, a marked decrease in serum lipids was obtained. Furthermore, a significant increase in feed conversion rate, leukocytic count, phagocytic activity, phagocytic index, serum total globulin, ? globulin and malondialdehyde coupled with a marked increase in ? and ? globulins were determined. Medication of infected broilers with lincomycin and/or bacitracin improved clinical signs and reduced mortality rate to 8, 6 and 2%, respectively, as well as restored the performance and hematobiochemical alterations.Conclusions: a combination of lincomycin and bacitracin was of considerable value for the control of necrotic enteritis in broiler chickens.

Acute generalized exanthematous pustulosis caused by lincomycin: a case report / 中华皮肤科杂志

A 28-year-old male patient with coughing was treated with intramuscular injection of lincomycin,oral Kesouting granules and erythromycin in a local clinic.One day later,erythema occurred on the head and face,and rapidly spread to the trunk and limbs.Three days later,a large number of densely distributed needle tip-to millet-sized pustules occurred on the generalized erythema all over the body with fever and burning pain sensation of the skin.Skin examination revealed diffuse edematous erythema with obvious hyperemia on more than 90％ of the body,a large number of needle tip-to millet-sized whiteyellowish pustules on the erythema on the hair line,face,flexor aspect of the extremities and flexural site of the trunk (axillary and inguinal regions),and bilateral lower-extremity swelling.No erythema or erosion was observed on the oral mucosa or genital mucosa.Histopathological examination of skin lesions on the right elbow showed local intraepidermal and subcorneal pustules,necrotic keratinocytes and neutrophil aggregation in the pustules,and infiltration of lymphocytes and eosinophils in the superficial dermis.Laboratory examination showed elevated white blood cell counts (26.9 × 109/L),neutrophils proportion (Segment,0.88),C-reactive protein level (127.89 rmg/L),aspartate aminotransferase level (44.2 U/L) and alanine transarninase level (77.3 U/L),but decreased proportion of lymphocytes (0.08).The patient was diagnosed with acute generalized exanthematous pustulosis.After admission,the patient was treated with intravenous drips of methylprednisolone at a dose of 60 mg/d.Then,the condition was rapidly relieved,and the dosage was rapidly reduced.The patient was discharged on day 7.

Effects of intestinal flora imbalance on pharmacokinetic parameters of baicalin and baicalein in rats / 中草药

Objective To study the effects of intestinal flora imbalance after ig administration on pharmacokinetic parameters of baicalin or baicalein in rats. Methods The SD rats were divided into four groups including baicalin group, antibiotic + baicalin group, baicalein group, and antibiotic + baicalein group. Traditional antibiotic medicine lincomyci were used to induce rats gut micro dysbiosis for 5 d. The pharmacokinetics of related technologies and methods were used, and the rats were administered with Moore dose (370 μmol/kg) of baicalin and baicalein. The plasma samples were collected at different time points within 20 h, and the concentration of baicalin was determined with LC-MS/MS, and the curve was drawn. The data were analyzed by DAS.2.2 software, comparison of baicalin and baicalein in animal behavior changes of rats in normal rats and antibiotics. Results The results showed that the baicalein was metabolized entirely and the metabolite baicalin was detected mainly in rat plasma after oral administration of baicalein. These results showed that the Cmax [ (7.80 ± 5.52) mg/L] of baicalin in rats in antibiotic + baicalin group was decreased compared with that with baicalin alone [Cmax (16.35 ± 9.48) mg/L]. Meanwhile, the AUC0~t of baicalin in antibiotic + baicalin group was 32.60 ± 18.88 mg∙h/L which was significantly lower than that in rats with baicalin alone [ (75.16 ± 48.40) mg∙h/L]. These results showed that the Cmax [ (10.28 ± 5.57) mg/L] of baicalin in rats of antibiotic + baicalein group was decreased compared with that with baicalein alone [Cmax (60.39 ± 56.32) mg/L]. Meanwhile, the AUC0~t of baicalin in antibiotic + baicalein group was (71.67 ± 54.49) mg∙h/L which was significantly lower than that in rats with baicalein alone [ (212.51 ± 101.25) mg∙h/L]. Conclusion Baicalin and baicalein showed bad pharmacokinetic behavior in rats when the rat intestinal flora is imbalance.

Statistical Modelling and Optimization of Fermentation Medium for Lincomycin Production by Streptomyces lincolnensis Immobilized Cells

ABSTRACT Response surface methodology was used to optimize lincomycin production by Streptomyces lincolnensis NRRL ISP-5355 in submerged fermentation. Screening of fermentation medium components to find their relative effect on lincomycin production was done using Plackett-Burman design. Malt extract, dextrin, soluble starch and (NH4)2SO4 were the most significant nutrient influenced on lincomycin production. Central composite design was applied to determine optimal concentrations of these factors and the effect of their mutual interactions. The interaction between soluble starch and (NH4)2SO4 was found to enhance the production, whereas malt extract and dextrin exhibited an influence independent from the other two factors. Using this statistical optimization method, maximum lincomycin concentration of 1345 μg/ml was obtained which represented a 40.5 % increase in titer than that acquired from the non-optimized medium. This statistically optimized medium was employed for lincomycin production through immobilization of Streptomyces lincolnensis by adsorption on synthetic cotton fibers. Immobilization technique improved the concentration to 1350 μg/ml higher than that produced from free cells cultures and could be maintained for longer than 17 days in a repeated batch system.

Medium Molecular Weight Chitosan as a Carrier for Delivery of Lincomycin Hydrochloride from Intra-pocket Dental Film: Design, Development, in vitro and ex vivo Characterization.

The purpose of investigation is to find out the potential of Medium Molecular Weight Chitosan (MMWCH) loaded with Lincomycin Hydrochloride (LNC) having pKa 7.6 and log p value 0.20 for treatment of periodontitis and gingivitis, prepared by using solvent casting technology in form of intra pocket dental film. Four sets of formulation were prepared and each set comprises of four formulations each. The formulations were evaluated for drug content uniformity, weight uniformity, thickness of patch, surface pH, moisture loss, swelling index, water vapor transmission rate, static in vitro release studies using diffusion cell, ex vivo flux study using diffusion cell by help of excised gum lining of goat, release kinetics and Akaike Information Criteria; goodness of fit (AIC) value determination. Excipient drug interaction was carried out by using Fourier Transform Infrared spectroscopy (FTIR), and by Thermo gravimetric Analysis (TGA)/Differential thermal analysis (DTA)/Derivative thermo gravimetric analysis (DTG) and this suggests that there is no drug excipient interaction occurs. The drug release studies show the sustained release without any burst effect for consecutive 5 days. Formulation R1, R2, R7, R8, R9, R10, R13 and R14 and follows the zero order release pattern and formulation R3, R4, R5, R6, R11, R12, R15 and R16 follows the Higuchi model because they have lower AIC value and higher r2 value. Formulation ER17, ER18, ER19 and ER20 is having the average flux of 1.0, 1.48, 1.35 and 1.45 mg/cm2 hr-1 respectively, and when compared statistically student’s paired t-test these all formulations are significantly different from each other.

Pharmacokinetics of ginsenoside Rb1 in lincomycin-induced gut microbiota dysbiosis rats / 中国药科大学学报

@#Gut microbiota-mediated deglycosylationplays an important role in the metabolism of ginsenoside Rb1. Thus, a lincomycin-induced gut microbiota dysbiosis rat model was selected to explored the pharmacokinetics and deglycosylation metabolism of ginsenoside Rb1. An UPLC-MS/MS analytical method was developed to detect ginsenoside Rb1 and its deglycosylated metabolite, Rd in rat plasma. The triple quadruple mass spectrometer was set in negative electrospray ionization mode by multiple reaction monitoring. The method was validated to meet the requirements of biological applications, by evaluating specificity, linearity, lower limits of quantification(LLOQ), precision, accuracy, matrix effect, recovery and stability. Gut microbiota dysbiosis rats were induced by oral administration of lincomycin(5 000 mg/kg)for 7 continuous days. The in vitro and in vivo results reveal that the reduced β-D-glucosidase activity significantly decreases the Rd formation rate in lincomycin-induced gut microbiota dysbiosis rats, leading to the pharmacokinetic alteration of ginsenoside Rb1 and Rd in gut microbiota dysbiosis rats.

Effect of Lincomycin on the Intestinal Mucosa Barrier of Mice / 医药导报

Objective To study the effect of lincomycin hydrochloride on the intestinal mucosal barrier of mice. Methods A total of 24 mice were equally and randomly divided into normal control group and model group. Mice in the model group were administered with 8 mg · kg-1 · d-1 of lincomycin hydrochloride through gastric lavage for 3 days to establish the model of intestinal mucosa injury and alteration of intestinal flora in mice. The intestinal flora was tested,bacterial translocation was analyzed,and mucosa permeability was determined by measuring diamine oxidase( DAO)in plasma. Results Lincomycin hydrochloride led to alteration of intestinal flora in mice after oral administration for three days in mice. The aerobes translocation rate was 16. 7% and 52. 3% in the normal and model groups,respectively(P〈0. 01). The anaerobes translocation rate was 8. 3% and 68. 2% in the normal and model groups,respectively(P〈0. 01). The plasma concentration of diamine oxidase was increased from(2. 08±0. 05)mg·mL-1 in the normal group to(7. 18±0. 10)mg·mL-1 in the model group(P〈0. 01). Conclusion Lincomycin hydrochloride damages intestinal mucosal barrier in mice.

Pruebas de sensibilidad frente a agentes anti microbianos en cepas de Brachyspira pilosicoli aisladas a partir de ponedoras comerciales en Colombia / Antimicrobial susceptibility test in Brachyspira pilosicoli strains isolated from commercial layers farms in Colombia

Las espiroquetas intestinales del género Brachyspira ocasionan enfermedades importantes en porcinos y aves. Se ha evidenciado un problema de incremento en la presentación de cepas resistentes a los antimicrobianos utilizados normalmente para tratar las espiroquetosis intestinales en porcinos, y esto podría ser aplicable a los aislamientos de aves. Hay muypocos reportes de sensibilidad antimicrobiana in vitro de cepas de Brachyspira spp. aisladas en aves. En este estudio se evaluó la sensibilidad de doce aislamientos de Brachyspira pilosicoli obtenidos de granjas de ponedoras comerciales a los agentes antimicrobianos tiamulina, tilosina y lincomicina, y se estableció la concentración mínima inhibitoria (CMI)mediante la técnica de dilución en agar. Todas las bacterias analizadas fueron sensibles a tiamulina (CMI≤0,1 μg/ml) y lincomicina (CMI 1 μg/ml) y resistentes a tilosina (CMI 5 μg/ml).

Intestinal Spirochaetes of the genus Brachyspira cause important diseases in swine and poultry. An increasing problem in the presentation of resistant strains to the antimicrobial drugs usually used to treat the intestinal spirochaetosis in swine has been evidenced and this could be applicable to the isolations from poultry. There are very few reports of in vitro antimicrobialsusceptibility of Brachyspira spp. isolated from birds. In this study the antimicrobial susceptibility of twelve Brachyspira pilosicoli isolates obtain from commercial layers was evaluated against tiamulin, tylosin and lincomycin establishing the Minimum Inhibitory Concentration (MIC) by agar dilution technique. All bacteria analyzed were sensitive to tiamulin (MIC ≤0,1μg/ml), and lincomycin (MIC 1μg/ml) and resistant to tylosin (MIC 5μg/ml).

Effect of lincomycin treatment of root surface in dental replantation: a study in rats / Efeito da lincomicina como tratamento da superfície radicular no reimplante de dentes: estudo em ratos

Purpose: The purpose of studies on antibiotics used topically on the root surface of avulsed teeth is to evaluate their antiresorptive properties which favor the repair of the periodontal ligament and the reestablishment of the dentoalveolar articulation. The aim of the present study was to determine the effect of lincomycin treatment of the root surface on tooth replantation. Methods: Ten rats were distributed into two groups (I - control; II - experimental). The right maxillary incisor of the animals was extracted and stored in milk for 30 min. The tooth in group I was rinsed with normal saline and replanted; in group II, the incisor was immersed in lincomycin for 5 min before replantation. The animals were euthanized on the 21st day postoperative. The right hemimaxilla was submitted to histological sectioning and stained with H&E for microscopic evaluation. Results: Group I: the periodontal ligament appeared dispersed, with moderate to intense lymphoplasmacytic infiltrate, and dentoalveolar articulation was not reestablished. Group II: complete repair of the ligament was evident, and there were few inflammatory cells and small areas of inflammatory resorption and ankylosis. Conclusion: The use of lincomycin allowed the repair of the periodontal ligament and reduced inflammation. There were still areas of inflammatory resorption and ankylosis.

Objetivo: Estudos sobre antibióticos usados topicamente na superfície radicular de dentes avulsionados buscam avaliar suas propriedades anti-reabsortivas que favoreçam o reparo do ligamento periodontal e o restabelecimento da articulação dentoalveolar. Neste mesmo propósito, esta pesquisa avaliou o efeito da lincomicina na superfície radicular, antes do reimplante. Metodologia: Dez ratos foram distribuídos em dois grupos de 05 animais (I - controle e II - experimental). O incisivo superior direito dos animais foi extraído e estocado em leite por 30 min. Em seguida, no grupo I, os dentes foram irrigados com soro fisiológico e reimplantados; no grupo II, os incisivos foram imersos em lincomicina por 5 min, antes do reimplante. Os animais foram eutanasiados no 21º dia pós-operatório e a hemimaxila direita submetida a cortes histológicos, corados em HE, para avaliação microscópica. Resultados: No grupo I, o ligamento periodontal apresentou-se disperso, com infiltrado linfoplasmocitário moderado a intenso e a articulação dentoalveolar não foi restabelecida; no grupo II, notou-se completo reparo do ligamento, poucas células inflamatórias e pequenas áreas de reabsorção inflamatória e anquilose. Conclusões: O uso tópico da lincomicina no tratamento da superfície radicular promoveu o reparo do ligamento periodontal, reduziu o processo inflamatório, mas ainda foram observadas áreas de reabsorção inflamatória e anquilose.

Preparation and Quality Control of Compound Lincomycin Nasal Drops for Children / 中国药房

OBJECTIVE: To prepare compound lincomycin nasal drops for children and establish a quality control method for this preparation. METHODS: Compound lincomycin nasal drops for children were prepared using lincomycin hydrochloride as main component with its content determined by polarimetry. The content and stability of the preparation within 12mon under room temperature were investigated. Meanwhile irritating test of rabbits' nasal mucosa was conducted. RESULTS: The prepared eye drops were limpid colorless liquid and it met the related standards stated in China Pharmacopeia(2005 edition) in identification as well as tests etc. Lincomycin hydrochloride showed a good linear relation in the range of 3.2～20.0mg?mL-1(r=0.999 9), with average recovery at 100.6%(RSD=0.69%). This preparation showed a little irritation on nasal mucosa, and it was stable within 12mon under room temperature. CONCLUSIONS: This preparation is simple and feasible in preparation technology and controllable in quality.

Improvement of the Determination Method of Main Component in Lincomycin Hydrochloride Eye Drops / 中国药房

OBJECTIVE:To improve the determination method for lincomycin hydrochloride eye drops so as to eliminate the interference of the bacterial inhibitor ethylparaben on the content of the main component.METHODS:The determination was performed by HPLC with phosphoric buffer (pH 6.8)-methanol (40∶ 60) as the mobile phase replacing the mobile phase of borax buffer (pH6.0)-methanol (4∶6) recommend in state chemicals standard technique (Method A).The contents of ethylparaben-contained sample and ethylparaben-free sample determined by HPLC were compared with those determined by Method A.RESULTS:There was no significant difference in the content of ethylparaben-free sample between the two determination methods,but the content of ethylparaben-contained sample determined by Method A was higher than both the labeled amount and that determined by the improved method.CONCLUSION:The improved method is applicable for the content determination of lincomycin hydrochloride eye drops.

Preparation and Content Determination of Lincomycin Hydrochloride Glycerol Paint / 中国药房

OBJECTIVE: To prepare lincomycin hydrochloride glycerol paint and to determine its content. METHODS: Lincomycin hydrochloride glycerol paint was prepared using lincomycin hydrochloride and dyclonine hydrochlorideas as main components; the contents of the two main components were determined by HPLC. RESULTS: The linear ranges of lincomycin hydrochloride and dyclonine hydrochloride were 20～200 ?g?mL-1(r=0.999 8) and 10～100 ?g?mL-1(r=0.999 9),respectively. The average recoveries(n=5) were 99.61% and 99.28%,with RSD stood at 0.439% and 0.818%,respectively. CONCLUSION: Both the preparative method and determination method for lincomycin hydrochloride glycerol paint are simple and feasible.

Therapeutic Effect of Topical Application of Linoleic Acid and Lincomycin in Combination with Betamethasone Valerate in Melasma Patients

Melasma is an acquired symmetric hypermelanosis characterized by irregular lightto gray-brown macules and patches on sun-exposed areas. Many therapeutic agents are available but are unsatisfactory. Recently, it has been demonstrated that lincomycin (LM) and linoleic acid (LA) can inhibit melanogenesis in vitro. Our purpose was to investigate the clinical efficacy of topical application of LM and LA in combination with betamethasone valerate (BV) in melasma patients. Fortyseven Korean female adults with clinically diagnosed melasma were enrolled in a 6-week, double-blind, randomized clinical trial. Patients were treated with one application of the vehicle (group A), 2% LM mixed with 0.05% BV (group B), or 2% LM mixed with 0.05% BV and 2% LA (group C) on the face every night. Determination of efficacy was based on the Melasma Area and Severity Index (MASI) score and objective assessment (no effect, mild, moderate, or excellent) at intervals of 2 weeks until the end of the study at 6 weeks. After 6 weeks, in comparison with the pre-treatment MASI score, the average MASI score of group C decreased to 68.9%, compared with 98% in group A (p<0.05) and 85.4% in group B. There was no statistically significant difference between group A and group B. Seven patients (43.7%) in group C revealed more than moderate improvement in objective assessment, compared with none in group A and two patients (12.5%) in group B. There were no significant side effects. Topical application of linoleic acid is considered to be effective in the treatment of melasma patients.